Composition for treatment of inflammatory disorders

Abstract

A pharmaceutical composition for parenteral administration, comprising liposomes composed of non-charged vesicle-forming lipids, optionally including not more than five (5) mole percent of charged vesicle-forming lipids, the liposomes having a selected mean particle diameter in the size range between about 40-200 nm and containing a water soluble corticosteroid for the site-specific treatment of inflammatory disorders, is provided.

1 . A pharmaceutical composition for parenteral administration comprising:
 non-charged liposomes consisting of cholesterol and partially or wholly synthetic non-charged vesicle-forming phospholipids, said liposomes having a selected mean particle diameter size range of between about 40 and about 200 nm, and   containing a corticosteroid for the site-specific treatment of an inflammatory disorder or disorders,   wherein the corticosteroid is present in water soluble form.   
   
   
       2 . A pharmaceutical composition for parenteral administration the pharmaceutical composition comprising:
 negatively charged liposomes consisting of cholesterol, partially or wholly synthetic non-charged vesicle-forming phospholipids and not more than 5 mol % negatively charged vesicle-forming phospholipids, the phospholipids having a selected mean particle diameter size range of between about 40 and about 200 nm and   containing a corticosteroid for the site-specific treatment of an inflammatory disorder or disorders,   wherein the corticosteroid is present in water soluble form.   
   
   
       3 . The pharmaceutical composition of  claim 1 , wherein the corticosteroid is a systemically administered corticosteroid. 
   
   
       4 . The pharmaceutical composition of  claim 3 , wherein the systemically administered corticosteroid in water soluble form is selected from the group consisting of prednisolone, dexamethasone, methylprednisolone, and mixtures thereof. 
   
   
       5 . (canceled) 
   
   
       6 . The pharmaceutical composition of  claim 5 , wherein the topically applied corticosteroid in water soluble form is selected from the group consisting of budesonide, flunisolide, fluticasone propionate, and mixtures thereof. 
   
   
       7 . A pharmaceutical composition for parenteral administration and site-specific treatment of an inflamed tissue, the pharmaceutical composition comprising:
 negatively charged liposomes consisting of cholesterol, partially or wholly synthetic non-charged vesicle-forming phospholipids, and not more than 5 mol % negatively charged vesicle-forming phospholipids, the phospholipids having a selected mean particle diameter size range of between about 40 and about 200 nm, and   containing a corticosteroid present in water soluble form,   wherein the pharmaceutical composition has a circulation half-life of at least 6 hours in a mammalian subject, and   further wherein the pharmaceutical composition exhibits increased localization and improved retention of corticosteroid after a single intravenous injection of the pharmaceutical composition at the inflamed tissue as may be determined by significant reversal of paw inflammation in a rat adjuvant arthritis model.